Use of 3,4-diphenyl chromans for the manufacture of a pharmaceutical composition for the treatment or prophylaxis of idiopathic or physiologic gynaecomastia

- Novo Nordisk A/S

The present invention provides novel uses of compounds of general formula I ##STR1## wherein R1, R4 and R5 are individually hydrogen, hydroxy, halogen, trifluoromethyl, lower alkyl, lower alkoxy or (tertiary amino)(lower alkoxy); and R2 and R3 are individually hydrogen or lower alkyl, or as a pharmaceutically acceptable salt thereof in combination with a pharmaceutically acceptable carrier for the manufacture of a pharmaceutical composition for the treatment or prophylaxis of idiopathic or physiologic gynaecomastia.

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Claims

1. A method for treatment or prevention of idiopathic or physiologic gynaecomastia comprising administering to a patient in need of such treatment a compound of formula I ##STR2## wherein R1, R4, and R5 are individually hydrogen, hydroxy, halogen, trifluoromethyl, lower alkyl, lower alkoxy or (tertiary amino)(lower alkoxy); and R2 and R3 are individually hydrogen or lower alkyl, or a pharmaceutically acceptable salt thereof in an amount sufficient to treat or prevent idiopathic or physiologic gynaecomastia.

2. The method according to claim 1 in which R1 is lower alkoxy, R2 and R3 are lower alkyl, R4 is hydrogen and R5 is tertiary amino lower alkoxy.

3. The method according to claim 1 wherein R1 is methoxy.

4. The method according to claim 1 wherein R2 is methyl.

5. The method according to claim 1 wherein R3 is methyl.

6. The method according to claim 1 wherein R4 is hydrogen.

7. The method according to claim 1 wherein R5 has the formula II: ##STR3##

8. The method according to claim 1 wherein said compound is an isolated d- or l-enantiomer.

9. The method according to claim 1 wherein said compound has the formula III:

10. The method according to claim 1 wherein said compound is an isolated l-enantiomer.

11. The method according to claim 1 wherein said compound is centchroman having the formula IV:

12. The method according to claim 11 wherein said compound is an isolated d- or l-enantiomer.

13. The method according to claim 11 wherein said compound is an isolated l-enantiomer.

14. The method according to claim 1 wherein said compound is administered orally.

15. The method according to claim 1 wherein said compound is administered in a range from about 0.001 to 75 mg/kg patient per day.

16. The method according to claim 1 wherein said compound is administered in the form of a dermal implant.

Referenced Cited
U.S. Patent Documents
3822287 July 1974 Bolger
4447622 May 8, 1984 Salman et al.
4895715 January 23, 1990 Neri et al.
5280040 January 18, 1994 Labroo et al.
5364847 November 15, 1994 Labrie et al.
Other references
  • Srivasta et al., "Mode of Action Of Centchroman At Vaginal And Ovarian Level In Immature Rats", Ind. J. Physiol. Pharmac, Jan.-Mar., 1980, vol. 24, pp. 44-48. Black et al., "Raloxifene (LY139481 HCI) Prevents Bone Loss and Reduces Serum Cholesterol Without Causing Uterine Hypertrophy In Ovariectomized Rats", J. Clin. Invest., vol. 93, Jan. 1994, pp. 63-69. Singh, MM, et al., Acta Endocrinologica, vol. 126, pp. 444-450, (1992).
Patent History
Patent number: 5919812
Type: Grant
Filed: Mar 4, 1997
Date of Patent: Jul 6, 1999
Assignee: Novo Nordisk A/S (Bagsvaerd)
Inventors: Niels Korsgaard (V.ae butted.rl.o slashed.se), Michael Shalmi (K.o slashed.benhavn V), Birgitte Hjort Guldhammer (Hiller.o slashed.d)
Primary Examiner: James H. Reamer
Attorneys: Steve T. Zelson, Esq., Cheryl H. Agris, Esq
Application Number: 8/811,154